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Anti-cancer medicine composition

An anti-cancer drug and composition technology, which can be used in drug combinations, anti-tumor drugs, pharmaceutical formulations, etc., can solve problems such as difficulty in forming effective drug concentrations, and achieve the effects of reducing DNA repair function and increasing sensitivity

Inactive Publication Date: 2005-07-06
DASEN BIOLOGICAL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor (see Kong Qingzhong "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (Kong Q et al., J Surg Oncol.1998 Oct; 69( 2): 76-82), simply increasing the dosage is limited by systemic reactions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] Put 80 mg of polylactic acid (PLA) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane to dissolve and mix well, add 10 mg of doxorubicin and 10 mg of topotecan, re-shake, and then vacuum-dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain an anticancer drug composition containing 10% by weight of doxorubicin and 10 mg of topotecan.

Embodiment 2

[0089] As described in Example 1, the difference is that the active ingredients are:

[0090] (a) 10% letotecan, irinotecan, etoposide, teniposide, camptothecin, 9-nitrocamptothecin (9NC), 7-ethyl-10-hydroxy-camptothecin Camptothecin, 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonylcamptothecin, 10-hydroxy-camptothecin, topotecan, (+)- 1,2-bis(3,5-dioxopiperazinyl)propane, m-2,3-bis(3,5-dioxopiperazin-1-yl)butane, bisdioxopiperazine Or N-[2-(dimethylamino)ethyl) aridine-4-carboxamide with 10% doxorubicin, mitomycin C, actinomycin D, mitoxantrone, dactinomycin, A combination of daunorubicin, bleomycin, zorblemycin, cyclosporine A, or neocarcinstatin; or

[0091] (b) 10% letotecan, irinotecan, etoposide, teniposide, camptothecin, 9-nitrocamptothecin (9NC), 7-ethyl-10-hydroxy-camptothecin Base, 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonylcamptothecin, 10-hydroxy-camptothecin, topotecan, (+)-1 , 2-bis(3,5-dioxopiperazinyl)propane, m-2,3-bis(3,5-dioxopiperazin-1-yl)buta...

Embodiment 3

[0095] Put 70 mg of polyglycolic acid and glycolic acid copolymer (PLGA) with a molecular weight of 10,000 into a container, add 100 ml of dichloromethane to dissolve and mix well, add 20 mg of doxorubicin and 10 mg of topotecan, re-shake and vacuum Dry to remove organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anticancer drug composition containing 20% ​​doxorubicin and 10% topotecan by weight. The anticancer drug composition was placed under the skin of mice, and the drug content was measured by taking it out regularly, and the cumulative release percentage (%) was calculated according to the remaining drug amount. It was found that 80-95% of the drug was released uniformly within 30 days. All are percentages by weight.

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PUM

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Abstract

An anticancer pharmaceutical composition composed of pharmaceutic adjuvant and enwrapped anticancer effective constituent is disclosed. Wherein, the anticancer effective constituent is a composition of tumor resistant antibiotic and ToPo enzyme inhibiting agent, the ToPo enzyme inhibiting agent can inhibit the intracellular DNA repairing function and can lower the tolerance of tumor cell to the tumor resistant antibiotic, while the pharmaceutic adjuvant can mainly be biological compatible, degradable and absorbable macromolecule polymer, which can make the anticancer drug release slowly to the local region of tumor in the degradation and absorption process, therefore both lowers considerably the whole body toxic reaction and sustains effective drug level in local region of tumor.

Description

(1) Technical field [0001] The invention relates to an anticancer drug composition, which belongs to the technical field of drugs. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among the various chemotherapeutic drugs used, the effect of antitumor antibiotics is more obvious, and has been widely used in many malignant tumors. Since anti-tumor antibiotics exert their anti-tumor effect by binding to DNA and inhibiting RNA synthesis, and the DNA repair function in many tumor cells increases significantly after treatment, effectively reducing or inhibiting the DNA repair function in tumor cells becomes focus of current research. [0003] It has recently been found that inactivation or inhibition of intracellular DNA repair proteins can enhance the sensitivity of some tumor cells to chemotherapy (see Dolan et al. ""Cancer Research" 51 pp. 3367-3372 (1991) (Dolan et al., Cancer Res., 51, 3367-3372, 1991)). However, ...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61P35/00
Inventor 孔庆忠
Owner DASEN BIOLOGICAL PHARMA CO LTD
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